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. 2019 Jan 25;10(2):332–340. doi: 10.1039/c8md00537k

Table 5. Inhibitory effects and IC50 of series II peptide-like ligand binding rhNRP-1 (chemiluminescence detection).

Compound AA2–AA3 fragment Inhibition of NRP-1/VEGF-A165 binding [%]
IC50 [μM]
100 μM 50 μM 25 μM 10 μM 5 μM 2.5 μM 1 μM
3 Dab–Pro 79.8 ± 0.8 76.6 ± 0.9 70.4 ± 0.5 58.6 ± 1.4 43.7 ± 0.7 31.4 ± 0.5 13.8 ± 0.3 8.9 ± 0.8 (ref. 40)
11 Dab–Hyp 78.6 ± 0.7 76.0 ± 0.6 67.3 ± 1.5 54.3 ± 2.0 36.0 ± 0.0 22.3 ± 1.5 22.5 ± 0.3 9.2 ± 0.7 a
12 Dab–Aze 78.8 ± 0.6 75.8 ± 0.3 69.1 ± 0.3 49.6 ± 4.2 30.1 ± 1.8 12.9 ± 1.4 7.7 ± 1.0 11.7 ± 1.2 b
13 Dab–ΔPro 87.1 ± 0.6 84.4 ± 0.3 78.1 ± 1.0 70.7 ± 0.3 58.0 ± 0.8 44.8 ± 0.4 29.9 ± 1.5 4.3 ± 0.2 c
14 Dab–Oic 83.0 ± 0.3 79.5 ± 0.5 77.7 ± 1.3 63.4 ± 1.9 52.3 ± 3.3 50.9 ± 3.2 37.7 ± 2.1 2.3 ± 0.2 d
15 Dab–Piz 51.8 ± 0.4 46.0 ± 0.6 34.8 ± 0.3 20.8 ± 0.6 80.5 ± 2.0 e
16 Dab–Tic 0.0 ± 3.2 17.2 ± 1.4 35.0 ± 1.2 31.5 ± 2.5 ≫100

alog IC50 = –5.03 ± 0.07.

blog IC50 = –4.97 ± 0.05.

clog IC50 = –5.54 ± 0.04.

dlog IC50 = –5.65 ± 0.08.

elog IC50 = –4.09 ± 0.07. R2 was between 0.92–0.98. Results are presented as the mean ± SEM.